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SY-5102 is a potent, selective, orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd of 0.03 nM. It exhibits antiproliferative activity against HCC70 cells with an EC50 of 9 nM. SY-5102 inhibits CDK7-mediated CAK function [downregulating CDK2Thr160 phosphorylation] and TFIIH transcription function [downregulating RNA polymerase II Ser5 phosphorylation]. The compound induces G2/M cell cycle arrest, downregulates the expression of the oncogene c-Myc, and ultimately triggers apoptosis in cancer cells. SY-5102 is applicable for research in triple-negative breast cancer (TNBC).
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | SY-5102 is a potent, selective, orally active cyclin-dependent kinase (CDK7) inhibitor with a Kd of 0.03 nM. It exhibits antiproliferative activity against HCC70 cells with an EC50 of 9 nM. SY-5102 inhibits CDK7-mediated CAK function [downregulating CDK2Thr160 phosphorylation] and TFIIH transcription function [downregulating RNA polymerase II Ser5 phosphorylation]. The compound induces G2/M cell cycle arrest, downregulates the expression of the oncogene c-Myc, and ultimately triggers apoptosis in cancer cells. SY-5102 is applicable for research in triple-negative breast cancer (TNBC). |
| Targets&IC50 | CDK7:0.03 nM (Kd) |
| Molecular Weight | 457.46 |
| Formula | C22H22F3N7O |
| Cas No. | 2365230-48-2 |
| Smiles | C(F)(F)(F)C=1C(C=2C=3C(NC2)=NC(=CC3)C=4C(C)=NOC4C)=NC(N[C@H]5CCCNC5)=NC1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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